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Submit ReviewRoscovitine is a cyclin-dependent kinase (cdk) inhibitor. Displays sub-micromolar inhibition of cdk1, cdk2, cdk5, cdk7 and cdk9 (reported IC50 values range from 0.16 - 0.28 μM for cdk5 to 0.8 μM for cdk7). Selective for cdks over a wide range of related kinases including ERK1 and ERK2. Arrests L1210 cells in G1 phase. Inhibits phosphorylation of vimentin in vivo. Antimitotic.
Roscovitine is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
M. Wt | 354.45 |
Formula | C19H26N6O |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 186692-46-6 |
PubChem ID | 160355 |
InChI Key | BTIHMVBBUGXLCJ-OAHLLOKOSA-N |
Smiles | OC[C@@H](CC)NC1=NC(N(C(C)C)C=N2)=C2C(NCC3=CC=CC=C3)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 35.44 | 100 | |
ethanol | 35.44 | 100 |
The following data is based on the product molecular weight 354.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.82 mL | 14.11 mL | 28.21 mL |
5 mM | 0.56 mL | 2.82 mL | 5.64 mL |
10 mM | 0.28 mL | 1.41 mL | 2.82 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
References are publications that support the biological activity of the product.
De Azevedo et al (1997) Inhibition of cyclin-dependent kinases by purine analogues. Eur.J.Biochem. 243 518 PMID: 9030780
Meijer (1996) Chemical inhibitors of cyclin-dependent kinases. Trends Cell.Biol. 6 393 PMID: 15157522
Meijer et al (1997) Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur.J.Biochem. 243 527 PMID: 9030781
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
If you know of a relevant reference for Roscovitine, please let us know.
Keywords: Roscovitine, Roscovitine supplier, , Tocris Bioscience
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